Cartisamine
Cartisamine Uses, Dosage, Side Effects, Food Interaction and all others data.
Ginkgo biloba extract contains a group of terpene lactones (notably, ginkgolides and diterpenes) and ginkgo flavone glycosides (notably, ginkgetin, bilobetin, and sciadopitysin) that have antioxidant and vasoactive properties. Most of the studies that investigate the effect of ginkgo biloba use the standardized extract of Ginkgo biloba (EGb) 761 (EGb761), which was developed by a German pharmaceutical company in 1964. EGb761 contains 6% terpene lactones and 24% flavonoid glycosides. Flavonoids include quercetin, rutin, kaempferol, and isorhamnetin. Lactones include ginkgolide A, ginkgolide B, ginkgolide C, bilobalide, and ginkgotoxin, a lactone that is structurally related to pyridoxine. Ginkgo biloba is an herbal plant that is now cultivated worldwide. It is originally native to China, and ginkgo biloba extract has been used in traditional Chinese medicine for centuries.
After its nootropic properties were discovered, ginkgo biloba has gained attention as a therapeutic ingredient for memory and concentration enhancement in cognitive impairment and neurogenerative diseases, such as dementia. Ginkgo biloba was investigated in preliminary studies for a variety of therapeutic purposes such as improving cardiovascular health, sexual dysfunction, psychiatric disorders, skin disorders, and glaucoma. Ginkgo biloba is found in a number of homeopathic and over-the-counter herbal products and dietary supplements, but it has no approved therapeutic indications by regulatory bodies, such as the FDA, EMA, and Health Canada. Ginkgo folium, the leaf extract of Ginkgo biloba, is considered an anti-dementia drug by the World Health Organization.
Ginkgo biloba is a herbal ingredient with demonstrated antioxidant, vasoactive, antiapoptotic, anti-inflammatory, antiplatelet, and fibrinolytic properties. Ginkgo biloba has been investigated for use in a variety of medical conditions, but the most extensively studied area is in the context of cognitive impairment and neurodegenerative disorders. Ginkgo biloba was examined as a potential nootropic agent or cognitive enhancer but research findings supporting the therapeutic efficacy of ginkgo biloba extract (EGb) in dementia remain controversial. Some clinical studies of dementia that were up to one year long showed that EGb improves the cognitive performance and social functioning of patients. However, other studies did not support its clinical benefit for patients with cognitive impairment and dementia. Numerous meta-analysis studies showed insufficient evidence of the effectiveness of EGb in reducing both all-cause dementia incidence and Alzheimer's disease-associated dementia incidence in elderly patients with normal cognition or with mild cognitive impairment. Additionally, there is no up-to-date evidence that demonstrates the benefit of the long-term use of standardized EGb in reducing the risk of progression to Alzheimer's disease. A 2012 meta-analysis did not support the use of EGb in enhancing cognitive function in healthy adults.
Glucosamine is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. Glucosamine stimulates the production of proteoglycans and increases sulfate uptake by articular cartilage.
The administration of glucosamine, in theory, provides a building block towards the synthesis of glycosaminoglycans, slowing the progression of osteoarthritis and relieving symptoms of joint pain. Studies to this date examining the efficacy of glucosamine sulfate have been inconclusive. Glycosaminoglycans contribute to joint cartilage elasticity, strength, and flexibility. A systematic review of various studies and guidelines determined that modest improvements were reported for joint pain and function in patients taking glucosamine. A consistent joint space narrowing was observed, but with an unclear clinical significance.
| Trade Name | Cartisamine |
| Generic | Glucosamine + Ginkgo Biloba |
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| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Ginkgo biloba is a herbal supplement found in over-the-counter or unapproved homeopathic products for various health conditions, such as cognitive, neurodegenerative, cardiovascular, and reproductive health disorders.
Ginkgo biloba does not currently have any approved therapeutic indications, and there is insufficient evidence to support its unapproved use. It is available in over-the-counter herbal products mostly for oral use, to improve memory and cognitive problems.
Indicated for the treatment of osteoarthritis of knee, hip, spine, and other locations. Also used as dietary supplement
Cartisamine is also used to associated treatment for these conditions: Cognitive Dysfunctions, Cognitive Function, DepressionArthritis, Backache, Joint Pain, Osteoarthritis (OA), Osteoarthritis of the Knee
How Cartisamine works
Two key active ingredients in ginkgo biloba are terpene lactones (notably ginkgolides and diterpenes) and ginkgo flavone glycosides (notably ginkgetin, bilobetin, and sciadopitysin), which are present at varying concentrations. Ginkgo biloba extract EGb 761 is the standardized extract of ginkgo biloba used in studies, which contains 6% terpenoids and 24% flavonoid glycosides. Animal studies have shown that ginkgo biloba works on several neurotransmitter pathways and brain structures. Flavones were shown to inhibit lipid peroxidation; inhibit the uptake of serotonin, dopamine, and norepinephrine; and inhibit platelet aggregation. Terpene lactones may also act as potent antagonists of the platelet-activating factor and may possess anti-ischemic and fibrinolytic effects. They were also shown to downregulate adrenal peripheral benzodiazepine receptors and increase adrenocorticotropic hormone levels. Ginkgo biloba also reversibly inhibits monoamine oxidase A; and modestly inhibits anticholinesterase activity, leading to enhanced cholinergic transmission in the brain.
Several studies suggest that ginkgo biloba exerts neuroprotective effects by reducing free radical production in the prefrontal cortex, which may explain its improvement on short-term memory. Ginkgo biloba extract acts as a free radical scavenger, protecting neurons from oxidative damage and apoptosis related to aging, cerebral ischemia, and neurodegenerative disorders. Ginkgo biloba also inhibits amyloid-β neurotoxicity and protects against hypoxic challenges and increased oxidative stress. One study showed that bilobalide, a terpene lactone, delays the onset of hypoxic glycolysis. Ginkgo biloba has the potential to regulate metabolism, stabilize the membrane, and promote vasodilation. In the arterial endothelium, EGb stimulated the release of endogenous relaxing factors, such as endothelium-derived relaxing factor and prostacyclin. In the inflammatory environment that causes tissue damage, EGb promoted nitric oxide production, leading to enhanced peripheral and cerebral blood flow.
The mechanism of action of glucosamine in joint health is unclear, however there are several possible mechanisms that contribute to its therapeutic effects. Because glucosamine is a precursor for glycosaminoglycans, and glycosaminoglycans are a major component of joint cartilage, glucosamine supplements may help to rebuild cartilage and treat the symptoms of arthritis. Some in vitro studies show evidence that glucosamine reduces inflammation via inhibition of interferon gamma and Nuclear factor kappa B subunit 65 (NF-κB p65), improving the symptoms of arthritis and joint pain. Clinical relevance is unknown at this time.
Dosage
Cartisamine dosage
500 mg tablet three times daily or as directed by the physician. A single dose of 1500 mg daily may also be effective. Obese individuals may need higher doses, based on body weight.
Side Effects
Safety studies with Glucosamine show no demonstrable toxicity. Rarely occurring side effects like mild & reversible intestinal flatulence are almost like placebo.
Toxicity
Oral LD50 of standardized extract in mice is 7730 mg/kg, which corresponds to 2300 mg/kg of active ingredients, 1900 mg/kg of flavone glycosides, and 464 mg/kg of terpene lactones. Intravenous LD50 is 1100 mg/kg.
No case of overdose has been reported so far. Cyanogenic glycosides found in raw ginkgo seeds are potentially toxic compounds; thus, contact or ingestion of ginkgo seeds can lead to serious reactions such as allergic skin reaction, including acute generalized exanthematous pustulosis, and convulsions. Ginkgo toxicity can manifest as bleeding, seizure, and serotonin syndrome. As there is no known antidote for ginkgo toxicity, treatment includes discontinuation of ginkgo and symptomatic and supportive care. Seizures may be attributed to ginkgotoxin, which can cause seizures at high doses.
The oral LD50 of glucosamine in rats is >5000 mg/kg. Symptoms of an overdose with glucosamine may include nausea, vomiting, abdominal pain, and diarrhea (common side effects of this drug). Severe and life-threatening hypersensitivity reactions to glucosamine may occur in patients with a shellfish allergy or asthma.
Precaution
Diabetics are advised to monitor blood glucose levels regularly while taking Glucosamine. No special studies were formed in patients with renal and/or hepatic insufficiency. The toxicological and pharmacokinetic profile of the product does not indicate limitations for these patients. However, administration to these patients with severe hepatic or renal insufficiency should be under appropriate medical supervision.
Interaction
There have been no reports of significant drug interactions ofGlucosamine with antibiotics, antidepressants, antihypertensives, nitrates, antiarrhythmics, anxiolytic, hypoglycaemic agents, anti-secretives.
Volume of Distribution
No data available.
Results of a pharmacokinetic study of 12 healthy volunteers receiving three daily consecutive oral administrations of glucosamine sulfate soluble powder demonstrated glucosamine distribution to extravascular compartments. Human pharmacokinetic data for glucosamine is limited in the literature, however, a large animal model study of horses revealed a mean apparent volume of distribution of 15.4 L/kg. Concentrations of glucosamine ranged from 9-15 microM after an intravenous dose, and 0.3-0.7 microM after nasogastric dosing. These concentrations remained in the range of 0.1-0.7 microM in the majority of horses 12 hours after dosing, suggesting effectiveness of a once-daily dose. In rats and dogs, radioactivity from a C-14 labeled dose of glucosamine is detected in the liver, kidneys, articular cartilage, and other areas.
Elimination Route
Studies assessed the pharmacokinetic parameters of terpene lactones, the main component of ginkgo biloba. Following oral administration of ginkgo biloba solution, the mean absolute bioavailability was 80% for ginkgolide A, 88% for ginkgolide B and 79% for biloalide. In an early rat study, about 60% of radiolabeled EGb 761 was absorbed with a Tmax of 1.5 hours. The highest amount of radioactivity was measured in the stomach and small intestine.
In another study, after a single oral dose of 120 mg EGb 761 in healthy volunteers, Cmax was 22.22 ± 4.57 ng/mL for ginkgolide A, 8.27 ± 1.82 ng/mL for ginkgolide B, and 54.42 ± 13.62 ng/mL for biloalide. AUC0-∞ was 121.35 ± 22.92 ng × h/mL for ginkgolide A, 59.88 ± 11.39 ng × h/mL for ginkgolide B, and 217.24 ± 44.07 ng × h/mL for biloalide. Tmax ranged from 1.17 to 1.54 hours for those three compounds.
In a pharmacokinetic study, glucosamine was 88.7% absorption by the gastrointestinal tract. Absolute oral bioavailability was 44%, likely due to the hepatic first-pass effect. In a pharmacokinetic study of 12 healthy adults receiving oral crystalline glucosamine, plasma levels increased up to 30 times the baseline levels and Cmax was 10 microM with a 1,500 mg once-daily dose. Tmax was about 3 hours. AUC was 20,216 ± 5021 after a 15,000 mg dose.
Half Life
Unpublished human data reports that after oral administration of 80 mg EGb 761, the half-life was four hours for ginkgolides A and six hours for ginkgolides B. The half-life of bilobalide was three hours after administration of 120 mg EGb 761 extract.
The estimated half-life for glucosamine is 15 hours after an oral dose. After a bolus intravenous injection of 1005 mg crystalline glucosamine sulfate, the parent drug has an apparent half life of 1.11 hours.
Clearance
No data available.
Elimination Route
At 72 hours following oral administration in rats, about 38% of the ginkgo biloba extract was excreted via expiration, 22% was excreted in urine, and 29% was excreted in feces. About 70% of ginkgolides A, 50% of ginkgolides B, and 30% of bilobalide were excreted unchanged in the urine.
Fecal excretion of glucosamine in a pharmacokinetic study was 11.3% within 120 hours after administration. Urinary elimination was found to be 1.19% within the first 8 hours post-administration.
Pregnancy & Breastfeeding use
Women who are pregnant or who could become pregnant should not supplement with glucosamine. Glucosamine has not been studied enough to determine their effects on a developing fetus. And no studies have evaluated the use of Glucosamine during pregnancy or lactation. It should be taken with caution and medical advice during pregnancy and lactation.
Contraindication
There are no known contraindications for Glucosamine. But proven hypersensitivity to Glucosamine is a contraindication.
Storage Condition
Should be stored in cool and dry place.
Innovators Monograph
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